Abstract
The two estrogen receptor subtypes, ERα and ERβ, play important roles in breast cancer. To develop an ERα imaging agent, we synthesized fluoropropyl pyrazole triol (FPPT, 2), an analog of our ERα-selective ligand PPT. FPPT retains the high ERα binding selectivity of its parent PPT. We prepared [ 18F]FPPT ( 18F-2) in high specific activity, but estrogen target tissue uptake in female rats was minimal and was not displaceable by unlabeled estradiol, probably because of the lipophilicity and triphenolic nature of FPPT.
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